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Macrocyclic pyrrolo[2,3-d]pyrimidines published by G1 Therapeutics.
|
|||
|---|---|---|---|
| Compound | 82 | 83 | 84 |
| R | Piperidin-3yl | Pyrrolodin-3yl | Morpholin-2yl |
| IC50 (µM) | |||
| CDK9/T | 0.0055 | 0.012 | 0.088 |
| CDK7/H | 13 | 12 | 61 |
| CDK6/D3 | 28 | 14 | >100 |
| CDK5/p25 | 35 | 19 | 43 |
| CDK5/p35 | 30 | 16 | 40 |
| CDK1/B1 | 4.4 | 5.6 | 31 |
| CDK2/A | 3.1 | 3.1 | 10 |
| CDK2/E | 13 | 12 | 26 |
| CDK3/E | 7.2 | 8.6 | 54 |
| CDK4/D1 | 2.9 | 2.3 | 27 |
CDK: cyclin-dependent kinase; IC50: half maximal inhibitory concentration.
